988 CHEMOTHERAPY NOV. 1971

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1 988 CHEMOTHERAPY NOV. 1971

2 VOL. 19 NO. 8 CHEMOTHERAPY 989 Effect of medium-ph and inoculum size on activity of SB-PC heart infusion agar, mcg/ml Sensitivity distribution of Staphylococci to SB-PC in surgical field. (54 strains)

3 CHEMOTHERAPY NOV Sensitivity distribution of E. coli to SB-PC in surgical field. MIC (mcg/ml) (51 strains) Cross resistance E.coli (51strains)

4 VOL. 19 NO. 8 CHEMOHTERAPY 991 Sensitivity distribution of Pseudomonas aeruginosa to SB-PC in surgical field. Sensitivity distribution of Proteus to SB-PC in surgical field. (20 strains)

5 992 CHEMOTHERAPY NOV Kinetics of penicillin-derivatives by various B-lactamase Protein binding of SB-PC *ultra- filtration method Medium agar for SB-PC(Takeda).

6 CHEMOTHERAPY 993 Serum levels of SB-PC Method; Cylinder plate method Test org.; B. sub. ATCC 6633 Medium; Agar for SB-PC (Takeda) 500 mg i. m. Serum levels of SB-PC Method; Cylinder Plate method Test org.; B. sub. ATCC 6633 Medium; Agar for SB-PC (Takeda) 1000 mg i. m. Serum levels of SB-PC Serum levels of SB-PC 500mg i. m. Metliod: Cylinder plate method Test org: B. sub. ATCC 6633 Medium: Agar for SB-PC (Takeda)

7 994 CHEMOTHERAPY NOV Urine concentrations of SB-PC 500 mg i. m. Average recovery 202 mg (40.4%) Urine concentrations of SB-PC 1000 mg i. m. Average recovery 690 mg (69.0%)

8 VOL. 19 NO. 8 CHEMOTHERAPY 995 Tissue concentration of SB-PC Tissue concentration of SB-PC Clinical responses from SB-PC

9 996 CHEMOTHERAPY NOV Clinical resposes from SB- PC Clinical responses from SB- PC

10 VOL. 19 NO. 8 CHEMOTHERAPY 997 1) NoviK, R. P. Biochem. J. 83 : 236, ) HENNESSEY, T. D. & M. H. RICHMOND: Biochem. J. 109 : 469, ) SAVATH, L. D. ; M. JAGO & E. P. ABRAHAM: Biochem. J. 96 : 739, ) TE-WENCHANG & Lows WEINSTEIN: Antimicr. Agents & Chemoth. 1963: 278

11 998 CHEMOTHERAPY NOV LABORATORY AND CLINICAL EVALUATION OF SULFOBENZYLPENICILLIN (SB-PC) SHUNJI ISHIYAMA, IKU KAWAKAMI, ISSEI NAKAYAMA, HIDEO IWAMOTO, SHIGETOMI IWAI, TOSHIHIKO OSHIMA, MUTSUMI TAKATORI, TAKAMICHI KAWABE, KUNIO SUZUKI, and FUJIYA MURAKAMI Department of Surgery, Nihon University, School of Medicine Laboratory and clinical studies were conducted on sulfobenzylpenicillin (SB-PC ). SB-PC showed MIC of 0. 8 `3. 12 mcg/ml against strains of Staphylococcus aureus and of `12. 5 against Escherichia coli strains. The antibacterial activity was a little lower than that of carbenicillin (CB-PC) and ampicillin (AB-PC) against Staph. aureus and almost the same as that of CB-PC and AB-PC against E. coli. The susceptibility of 54 clinical isolates of Staph. aureus to SB-PC ranged from ` 100 mcg/ml in MIC. Fourty-nine of the 54 isolates were susceptible to `12. 5 mcg/ml of SB-PC. While, the 51 clinical isolates of E. coli were susceptible to SB-PC in the range of ` 100 mcg/ ml, 38 of the 51 isolates being in the range of `50 mcg/ml. Cross resistance was recognized between SB-PC and CB-PC. The blood level of SB-PC following i. m. injection in man in dose of 500 mg, showed a mean peak value of mcg/ml 30 minutes after administration, decreasing gradually to 7. 5 mcg/ ml at 2 hours and 2. 0 mcg/ml at 6 hours. In dose of 1000 mg, i. m., the level exhibited a mean peak of 29.6 mcg/ ml at 30 minutes which decreased to 2.9 mcg/ml at 6 hours. The concentration of SB-PC in urine was highest (1000 `3000 mcg/ml) at 1 ` 2 hours after administration of 500 mg, i. m. The urinary recovery within 6 hours was 40. 4% for 500mg i. m. administration and 69% for 1000 mg. SB-PC given to rats in dose of 20 mg/kg was distributed into liver and kidneys at high concentrations. It was also found in lungs at high concentrations. In dose of 200 mg/kg, the results were similar to these. Twenty-one patients with surgical infections were treated with SB-PC. The treatment was successful in 15patients and not 3. The response was undeterminable in the remaining 3 cases. Three of the 21 cases complained of severe pain at the site of injection.

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